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    Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals
    4.
    发明授权
    Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
    四氢 - 苯并噻唑，其制备方法及其作为中间产物或药物的用途

    公开(公告)号：US4886812A

    公开(公告)日：1989-12-12

    申请号：US256671

    申请日：1988-10-12

    申请人： Gerhart Griss, deceased ,  Claus Schneider ,  Rudolf Hurnaus ,  Walter Kobinger ,  Ludwig Pichler ,  Rudolf Bauer ,  Joachim Mierau ,  Dieter Hinzen ,  Gunter Schingnitz

    发明人： Gerhart Griss, deceased ,  Claus Schneider ,  Rudolf Hurnaus ,  Walter Kobinger ,  Ludwig Pichler ,  Rudolf Bauer ,  Joachim Mierau ,  Dieter Hinzen ,  Gunter Schingnitz

    IPC分类号： A61K31/425 ,  C07D277/82

    CPC分类号： C07D277/82

    摘要： This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nucleic may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by fluorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.

    摘要翻译： 本发明涉及通式为（I）的新的四氢苯并噻唑，其中R 1表示氢原子，烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而上述苯基核酸 可各自被1或2个卤素原子取代，R2表示氢原子或烷基，R3表示氢原子，烷基，环烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基 基团可以被氟，氯或溴原子取代，R4表示氢原子，烷基，烷基或烯基，或者R3和R4与它们之间的氮原子一起代表吡咯烷子基，哌啶子基， 六亚甲基亚氨基或吗啉代基，其对映异构体及其酸加成盐。 上述通式I的化合物，其中R1或R3基团或R1和R3两个基团之一表示酰基，是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。 新化合物可以使用本身已知的方法制备。

    Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals
    5.
    发明授权
    Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
    四氢 - 苯并噻唑，其制备方法及其作为中间产物或药物的用途

    公开(公告)号：US4731374A

    公开(公告)日：1988-03-15

    申请号：US810947

    申请日：1985-12-19

    申请人： Gerhart Griss, deceased ,  Rudolf Hurnaus ,  Walter Kobinger ,  Ludwig Pichler ,  Rudolf Bauer ,  Joachim Mierau ,  Dieter Hinzen ,  Gunter Schingnitz

    发明人： Gerhart Griss, deceased ,  Rudolf Hurnaus ,  Walter Kobinger ,  Ludwig Pichler ,  Rudolf Bauer ,  Joachim Mierau ,  Dieter Hinzen ,  Gunter Schingnitz

    IPC分类号： A61K31/425 ,  C07D277/82

    CPC分类号： C07D277/82

    摘要： This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.

    摘要翻译： 本发明涉及通式为（I）的新的四氢苯并噻唑，其中R 1表示氢原子，烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而上述苯基核 可各自被1或2个卤素原子取代，R2表示氢原子或烷基，R3表示氢原子，烷基，环烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基 基团可以被氟里酰，氯或溴原子取代，R4表示氢原子，烷基，烷基或烯基，或者R3和R4与它们之间的氮原子一起代表吡咯烷子基，哌啶子基， 六亚甲基亚氨基或吗啉代基，其对映异构体及其酸加成盐。 上述通式I的化合物，其中R1或R3基团或R1和R3两个基团之一表示酰基，是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。 新化合物可以使用本身已知的方法制备。

    Fused-ring amino-pyrazines as bradycardiac agents
    6.
    发明授权
    Fused-ring amino-pyrazines as bradycardiac agents 失效
    稠环氨基吡嗪作为心动过缓剂

    公开(公告)号：US4409220A

    公开(公告)日：1983-10-11

    申请号：US297024

    申请日：1981-08-27

    申请人： Rudolf Hurnaus ,  Gerhart Griss ,  Robert Sauter ,  Wolfgang Grell ,  Walter Kobinger ,  Ludwig Pichler

    发明人： Rudolf Hurnaus ,  Gerhart Griss ,  Robert Sauter ,  Wolfgang Grell ,  Walter Kobinger ,  Ludwig Pichler

    IPC分类号： A61K31/495 ,  A61K31/55 ,  A61P9/02 ,  A61P9/06 ,  A61P9/12 ,  A61P25/02 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Compounds of the formula ##STR1## wherein A and B, which may be the same or different, each represent methylene, (alkyl of 1 to 3 carbon atoms)-methylene, ethylene or (alkyl of 1 to 3 carbon atoms)-ethylene;R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, alkenyl of 3 to 6 carbon atoms, phenyl-(alkyl of 1 to 3 carbon atoms), halophenyl-(alkyl of 1 to 3 carbon atoms), alkanoyl of 1 to 3 carbon atoms, phenyl-(alkanoyl of 1 to 3 carbon atoms), halophenyl-(alkanoyl of 1 to 3 carbon atoms), alkoxycarbonyl of 2 to 4 carbon atoms, aralkoxycarbonyl of 8 to 10 carbon atoms or phenyl;one of R.sub.2 and R.sub.3 is amino and the other is hydrogen, chlorine, bromine, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkoxycarbonyl of 2 to 4 carbon atoms, phenyl or halophenyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.

    摘要翻译： 其中A和B可以相同或不同，各自表示亚甲基，（1至3个碳原子的烷基） - 亚甲基，亚乙基或（1至3个碳原子的烷基） - 亚乙基; R 1是氢，1至6个碳原子的烷基，3至7个碳原子的环烷基，3至6个碳原子的烯基，苯基 - （1至3个碳原子的烷基），卤代苯基 - （1至3个碳原子的烷基 ），1〜3个碳原子的烷酰基，1〜3个碳原子的苯基 - （烷酰基），1〜3个碳原子的卤代苯基 - （烷酰基），2〜4个碳原子的烷氧基羰基，8〜10个碳原子的芳烷氧羰基， 苯基; R2和R3中的一个是氨基，另一个是氢，氯，溴，1至3个碳原子的烷基，1至3个碳原子的烷氧基，2至4个碳原子的烷氧基羰基，苯基或卤代苯基; 和无毒的，药学上可接受的酸加成盐。 化合物及其盐可用作心动过缓。

    Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals
    9.
    发明授权
    Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
    四氢 - 苯并噻唑，其制备方法及其作为中间产物或药物的用途

    公开(公告)号：US4843086A

    公开(公告)日：1989-06-27

    申请号：US124197

    申请日：1987-11-23

    申请人： Gerhart Griss, deceased ,  Claus Schneider ,  Rudolf Hurnaus ,  Walter Kobinger ,  Ludwig Pichler ,  Rudolf Bauer ,  Joachim Mierau ,  Dieter Hinzen ,  Gunter Schingnitz

    发明人： Gerhart Griss, deceased ,  Claus Schneider ,  Rudolf Hurnaus ,  Walter Kobinger ,  Ludwig Pichler ,  Rudolf Bauer ,  Joachim Mierau ,  Dieter Hinzen ,  Gunter Schingnitz

    IPC分类号： A61K31/425 ,  C07D277/82

    CPC分类号： C07D277/82

    摘要： This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms.R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by fluorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.

    摘要翻译： 本发明涉及通式为（I）的新的四氢苯并噻唑，其中R 1表示氢原子，烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而上述苯基核 可各自被1或2个卤素原子取代。 R2表示氢原子或烷基，R3表示氢原子，烷基，环烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而苯基核可以被氟取代 ，氯或溴原子，R4表示氢原子，烷基，烷基或烯基或R3和R4以及它们之间的氮原子表示吡咯烷子基，哌啶子基，六亚甲基亚氨基或吗啉代基，对映体和酸加成 的盐。 上述通式I的化合物，其中R1或R3基团或R1和R3两个基团之一表示酰基，是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。 新化合物可以使用本身已知的方法制备。

    Azepine derivatives and their anti-thrombotic compositions and methods
    10.
    发明授权
    Azepine derivatives and their anti-thrombotic compositions and methods 失效
    Azepine衍生物及其抗血栓形成和方法

    公开(公告)号：US4414225A

    公开(公告)日：1983-11-08

    申请号：US348496

    申请日：1982-02-12

    申请人： Robert Sauter ,  Gerhart Griss ,  Wolfgang Grell ,  Rudolf Hurnaus ,  Bernhard Eisele ,  Walter Haarmann ,  Eckhard Rupprecht

    发明人： Robert Sauter ,  Gerhart Griss ,  Wolfgang Grell ,  Rudolf Hurnaus ,  Bernhard Eisele ,  Walter Haarmann ,  Eckhard Rupprecht

    IPC分类号： C07D487/02 ,  A61K31/55 ,  A61P3/06 ,  A61P7/02 ,  C07D223/06 ,  C07D487/04 ,  C07D491/02 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/40

    CPC分类号： C07D487/04 ,  C07D223/06 ,  C07D491/04 ,  C07D495/04

    摘要： Compounds of the formula ##STR1## wherein n and m are each 1, 2 or 3, and the sum of n+m is 4;R.sub.1 is alkyl; alkenyl; unsubstituted, mono- or di-substituted aralkyl; unsubstituted, mono- or di-substituted benzoyl; alkoxycarbonyl; aralkoxycarbonyl; or, when m and n are each 2 and/or R.sub.2 and R.sub.3 are other than both hydrogen at the same time, also hydrogen;one of R.sub.2 and R.sub.3 is hydrogen or amino, and the other is carboxyl or alkoxycarbonyl; or, when R.sub.3 is hydrogen,R.sub.2 is hydrogen; amino; alkoxycarbonyl-amino; (unsubstituted or mono-substituted phenyl)-aminocarbonyl-; (unsubstituted or mono-substituted phenyl)ethylaminocarbonyl; azidocarbonyl; or hydrazinocarbonyl;X is oxygen, sulfur or ##STR2## where R.sub.4 is hydrogen; alkyl; phenyl-alkyl; or phenyl; non-toxic, pharmacologically acceptable acid addition salts thereof; and, when R.sub.2 or R.sub.3 is carboxyl, non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antithrombotics.

    摘要翻译： 其中n和m各自为1,2或3，并且n + m的和为4; R1是烷基; 烯基; 未取代的，单或二取代的芳烷基; 未取代的，单或二取代的苯甲酰基; 烷氧基羰基 芳烷氧羰基; 或者当m和n各自为2和/或R 2和R 3不同时为氢时，也为氢; R2和R3之一是氢或氨基，另一个是羧基或烷氧基羰基; 或当R3为氢时，R2为氢; 氨基; 烷氧基羰基 - 氨基; （未取代或单取代的苯基） - 氨基羰基 - ; （未取代或单取代的苯基）乙基氨基羰基; 叠氮羰基; 或肼基羰基; X是氧，硫或者其中R 4是氢; 烷基; 苯基 - 烷基; 或苯基; 无毒，药理学上可接受的酸加成盐; 并且当R 2或R 3为羧基时，与无机或有机碱形成的无毒的药学上可接受的盐。 化合物及其盐可用作抗血栓形成剂。